Transmucosal administration of 2,3-dimethoxy-5-methyl-6-(10-hydroxydecyl)-1,4-benzoquinone

a technology of idebenone and methyl-6, which is applied in the direction of antinoxious agents, drug compositions, metabolism disorders, etc., can solve the problems of poor the requirement for oral formulations of idebenone to be swallowed inflicts difficulties in the practical administration of patients with swallowing problems, and the dermal administration route has strong limitations regarding the administrable dose for systemic use, patient compliance and dosing accuracy

Inactive Publication Date: 2009-08-20
SANTHERA PHARMA SCHWEIZ
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Said high doses can result in unwanted side effects such as diarrhea.
In addition, the requirement for oral formulations of idebenone to be swallowed inflicts difficulties in the practical administration to patients with swallowing problems, e.g. a patient with a serious disease such as Duchenne Muscular Dystrophy or Friedreich's Ataxia, elderly or young patients.
However, the dermal administration route has strong limitations regarding an administrable dose for systemic use, patient compliance and dosing accuracy.

Method used

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  • Transmucosal administration of 2,3-dimethoxy-5-methyl-6-(10-hydroxydecyl)-1,4-benzoquinone
  • Transmucosal administration of 2,3-dimethoxy-5-methyl-6-(10-hydroxydecyl)-1,4-benzoquinone
  • Transmucosal administration of 2,3-dimethoxy-5-methyl-6-(10-hydroxydecyl)-1,4-benzoquinone

Examples

Experimental program
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Effect test

example 1

Micro-Emulsion Formulation

[0031]

TABLE 1Ingredient[mg / ml]FunctionIdebenone20Active IngredientMiglyol 812 N144SolventTPGS96SurfactantWater750Solvent

[0032]Preparation: TPGS (Tocopherol-polyethylenglycol-400-succinate) is preheated to about 60° C. Miglyol 812 N and idebenone are mixed and sonicated for approx. 10 minutes until the substance is completely dissolved (clear orange solution). The molten TPGS is added to the Miglyol / idebenone solution and stirred. The mixture is diluted and homogenized until a homogeneous emulsion is obtained.

example 2

Sublingual Tablet

[0033]

TABLE 2Ingredient[mg / tablet]FunctionIdebenone10Active IngredientLactose monohydrate60FillerPovidone K304.5BinderCroscarmellose5DisintegrantMicrocrystalline cellulose30FillerFlavour2.5Flavouring agentAspartame6SweetenerMagnesium stearate0.75GlidantTalc1.25Glidant

[0034]Preparation: Idebenone, lactose monohydrate, flavor and aspartame are mixed in a high-shear mixer until a homogeneous mixture is obtained. Povidone is dissolved in water (approx. 8-10% solution) and added to the dry mixture and granulated. The wet granules are dried in a fluid bed dryer, sieved and added to a pre-mixture of microcrystalline cellulose, magnesium stearate and talc. The final mixture is compressed to tablets.

example 3

Spray Formulation

[0035]

TABLE 3IngredientamountFunctionIdebenone10gActiveMethylparahydroxybenzoate2gPreservativePropylparahydroxybenzoate0.2gPreservativeAspartame0.6gSweetenerFlavour0.6gFlavouring agentEthanol (96%)500mlSolventPurified waterq.s.Solvent

[0036]Preparation: 10 g Idebenone is dissolved in 500 ml ethanol (96%) and is mixed with 400 ml of purified water. Methylparahydroxy benzoate, propylparahydroxy benzoate and aspartame are dissolved in the mixture. The final volume is adjusted to 1000 ml with purified water. The solution is filtered and filled into an appropriate spray device.

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Abstract

Use of idebenone for the preparation of a medicament for transmucosal administration.

Description

[0001]The present invention relates to a medicament for transmucosal administration of 2,3-dimethoxy-5-metriyl-6-(10-hydroxydecyl)-1,4-benzoquinone (idebenone).BACKGROUND OF THE INVENTION[0002]Idebenone is a synthetic analogue of coenzyme Q10 (CoQ10), a vital cell membrane antioxidant and essential constituent of the adenosine-triphosphate (ATP) producing mitochondrial electron transport chain (ETC). Up to now, idebenone has been used in a variety of medical applications. Similar to coenzyme Q10, idebenone undergoes reduction / oxidation cycles in living organisms and reduced idebenone is an antioxidant and radical scavenger (A. Mordente, G. E. Martorana, G. Minotti, B. Giardina, Chem. Res. Toxicol. 11 (1998), 54-63). It is known that idebenone protects cell membranes and mitochondria from oxidative damage because of its ability to inhibit lipid peroxidation (M. Suno, M. Shibota, A. Nagaoka, Arch. Gerontol. Geriatr. 8 (1989), 307-311). Idebenone also interacts with the ETC, preserving...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/68A61K31/122A61P25/28
CPCA61K31/122A61P21/00A61P21/04A61P25/00A61P25/16A61P25/28A61P27/02A61P3/00A61P3/12A61P39/06A61P43/00A61P9/00A61P9/10
Inventor DUBACH-POWELL, JUDITHHAUSMANN, RUDOLFVANKAN, PIERRE
Owner SANTHERA PHARMA SCHWEIZ
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